Detrol LA 4mg Capsules
It is used to treat an overactive bladder.
Drug Class
Urinary Antispasmodic
Pharmacologic Class
Antimuscarinic Agent
Pregnancy Category
Category C
FDA Approved
Sep 2000
DEA Schedule
Not Controlled
Overview
What is this medicine?
Detrol LA is a medication used to treat overactive bladder. It helps reduce symptoms like needing to go to the bathroom very often, feeling a sudden strong urge to urinate, and leaking urine. It works by relaxing the bladder muscle.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided to you and follow the instructions closely. You can take this medication with or without food, and it's best to take it at the same time every day. Continue taking the medication as directed by your doctor or healthcare provider, even if you're feeling well.
When taking your medication, swallow the tablet whole - do not chew, open, or crush it. Take it with a full glass of water to help the medication go down smoothly.
Storing and Disposing of Your Medication
To keep your medication effective and safe, store it at room temperature, away from light and moisture. Avoid storing it in a bathroom, as the humidity can affect the medication. Keep all medications in a secure location, out of the reach of children and pets.
What to Do If You Miss a Dose
If you miss a dose, skip it and take your next dose at the usual time. Do not take two doses at the same time or take extra doses to make up for the missed one. Stay on your regular schedule to maintain the effectiveness of your medication.
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided to you and follow the instructions closely. You can take this medication with or without food, and it's best to take it at the same time every day. Continue taking the medication as directed by your doctor or healthcare provider, even if you're feeling well.
When taking your medication, swallow the tablet whole - do not chew, open, or crush it. Take it with a full glass of water to help the medication go down smoothly.
Storing and Disposing of Your Medication
To keep your medication effective and safe, store it at room temperature, away from light and moisture. Avoid storing it in a bathroom, as the humidity can affect the medication. Keep all medications in a secure location, out of the reach of children and pets.
What to Do If You Miss a Dose
If you miss a dose, skip it and take your next dose at the usual time. Do not take two doses at the same time or take extra doses to make up for the missed one. Stay on your regular schedule to maintain the effectiveness of your medication.
Lifestyle & Tips
- Take the capsule whole; do not chew, crush, or break it.
- Take with or without food, as directed by your doctor.
- Maintain adequate fluid intake to prevent constipation and dry mouth.
- Avoid activities requiring mental alertness (e.g., driving, operating machinery) until you know how this medication affects you, as it may cause dizziness or blurred vision.
- Limit alcohol consumption, as it may worsen dizziness or drowsiness.
- Inform your doctor about all other medications you are taking, including over-the-counter drugs and herbal supplements.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
4 mg orally once daily
Dose Range:
2 - 4 mg
Condition-Specific Dosing:
concomitant_strong_cyp3a4_inhibitors:
2 mg orally once daily
hepatic_impairment:
2 mg orally once daily
renal_impairment_crcl_10_30_ml_min:
2 mg orally once daily
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed (CrCl > 30 mL/min)
Moderate:
2 mg orally once daily (CrCl 10-30 mL/min)
Severe:
2 mg orally once daily (CrCl < 10 mL/min) or avoid use due to limited data
Dialysis:
Consider 2 mg orally once daily; use with caution due to limited data
Hepatic Impairment:
Mild:
2 mg orally once daily
Moderate:
2 mg orally once daily
Severe:
2 mg orally once daily
Pharmacology
Mechanism of Action
Tolterodine is a competitive muscarinic receptor antagonist. It exerts its effect by blocking muscarinic receptors, primarily M2 and M3 subtypes, in the bladder, leading to inhibition of detrusor muscle contraction. This action reduces bladder pressure, increases bladder capacity, and decreases the frequency of involuntary detrusor contractions, thereby alleviating symptoms of overactive bladder such as urinary urgency, frequency, and urge incontinence.
Pharmacokinetics
Absorption:
Bioavailability:
17% (extensive metabolizers), 65% (poor metabolizers)
Tmax:
2-4 hours (for tolterodine and 5-hydroxymethyl metabolite)
FoodEffect:
Food increases AUC and Cmax by approximately 20% for tolterodine and 5-hydroxymethyl metabolite, but this is not considered clinically significant.
Distribution:
Vd:
113 L (tolterodine), 134 L (5-hydroxymethyl metabolite)
ProteinBinding:
96% (tolterodine), 50% (5-hydroxymethyl metabolite)
CnssPenetration:
Limited
Elimination:
HalfLife:
6-10 hours (tolterodine), 15-20 hours (5-hydroxymethyl metabolite)
Clearance:
Not available
ExcretionRoute:
Urine (77%), Feces (17%)
Unchanged:
Less than 1% (tolterodine), 5-14% (5-hydroxymethyl metabolite)
Pharmacodynamics
OnsetOfAction:
Within 1 week (clinical effect)
PeakEffect:
Within 4-8 weeks (maximal clinical effect)
DurationOfAction:
24 hours (due to extended-release formulation)
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Trouble passing urine
Changes in eyesight
Angioedema, a severe reaction that can be life-threatening, characterized by:
+ Swelling of the hands, face, lips, eyes, tongue, or throat
+ Trouble breathing
+ Trouble swallowing
+ Unusual hoarseness
If you experience any of these symptoms, get medical help right away.
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. Contact your doctor or seek medical help if you experience any of the following side effects or if they bother you or do not go away:
Feeling dizzy or sleepy
Headache
Stomach pain
Constipation
Dry mouth
Dry eyes
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Trouble passing urine
Changes in eyesight
Angioedema, a severe reaction that can be life-threatening, characterized by:
+ Swelling of the hands, face, lips, eyes, tongue, or throat
+ Trouble breathing
+ Trouble swallowing
+ Unusual hoarseness
If you experience any of these symptoms, get medical help right away.
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. Contact your doctor or seek medical help if you experience any of the following side effects or if they bother you or do not go away:
Feeling dizzy or sleepy
Headache
Stomach pain
Constipation
Dry mouth
Dry eyes
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe constipation or abdominal pain
- Difficulty urinating or inability to urinate (urinary retention)
- Severe blurred vision or eye pain
- Signs of an allergic reaction (rash, hives, swelling of face/lips/tongue, difficulty breathing)
- Chest pain or irregular heartbeat
- Confusion or hallucinations
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
Certain health conditions, including:
+ Urinary retention (trouble passing urine)
+ Glaucoma
+ Gastrointestinal issues, such as slow stomach emptying
Pre-existing kidney disease or liver disease
This list is not exhaustive, and it is crucial to discuss all your health problems and medications with your doctor.
To ensure safe treatment, provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter (OTC) medications you are taking
Natural products and vitamins you are using
Any health problems you have
Do not initiate, stop, or modify the dosage of any medication without first consulting your doctor to confirm that it is safe to do so in conjunction with this medication.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
Certain health conditions, including:
+ Urinary retention (trouble passing urine)
+ Glaucoma
+ Gastrointestinal issues, such as slow stomach emptying
Pre-existing kidney disease or liver disease
This list is not exhaustive, and it is crucial to discuss all your health problems and medications with your doctor.
To ensure safe treatment, provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter (OTC) medications you are taking
Natural products and vitamins you are using
Any health problems you have
Do not initiate, stop, or modify the dosage of any medication without first consulting your doctor to confirm that it is safe to do so in conjunction with this medication.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
Until you are aware of how this drug affects you, it is recommended that you avoid operating a vehicle or engaging in any activities that require alertness and clear vision.
Before consuming alcohol, using marijuana or other cannabis products, or taking any prescription or over-the-counter medications that may cause drowsiness or impair your reactions, consult with your doctor.
If you are pregnant, planning to become pregnant, or are breastfeeding, notify your doctor. You and your doctor will need to discuss the potential benefits and risks of this medication to both you and your baby.
Until you are aware of how this drug affects you, it is recommended that you avoid operating a vehicle or engaging in any activities that require alertness and clear vision.
Before consuming alcohol, using marijuana or other cannabis products, or taking any prescription or over-the-counter medications that may cause drowsiness or impair your reactions, consult with your doctor.
If you are pregnant, planning to become pregnant, or are breastfeeding, notify your doctor. You and your doctor will need to discuss the potential benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- Severe anticholinergic effects (e.g., severe dry mouth, dilated pupils, blurred vision, hot and dry skin, fever)
- Urinary retention
- Constipation
- Central nervous system excitation (e.g., restlessness, confusion, hallucinations, seizures)
- Tachycardia
- QT prolongation
What to Do:
Seek immediate medical attention. Contact a poison control center (Call 1-800-222-1222). Treatment is symptomatic and supportive. Gastric lavage may be performed. Physostigmine may be considered for severe central anticholinergic effects. ECG monitoring is recommended due to potential for QT prolongation.
Drug Interactions
Major Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, nelfinavir): Increased exposure to tolterodine, especially in poor CYP2D6 metabolizers. Dose reduction of tolterodine is required.
- Drugs that prolong QT interval (e.g., quinidine, sotalol, procainamide, amiodarone, pimozide, thioridazine, ziprasidone, moxifloxacin, erythromycin, tricyclic antidepressants): Potential for additive QT prolongation, especially in patients with pre-existing cardiac conditions.
Moderate Interactions
- Other anticholinergic agents (e.g., atropine, dicyclomine, oxybutynin, solifenacin): Additive anticholinergic effects (dry mouth, constipation, urinary retention, blurred vision).
- Prokinetic agents (e.g., metoclopramide, cisapride): Tolterodine may antagonize the effects of prokinetic agents due to its anticholinergic activity on GI motility.
- CYP2D6 inhibitors (e.g., fluoxetine, paroxetine, quinidine): May increase exposure to tolterodine, particularly in extensive metabolizers, but less pronounced than with CYP3A4 inhibitors.
Minor Interactions
- Warfarin: No significant interaction reported, but monitor INR if co-administered.
Monitoring
Baseline Monitoring
Assessment of urinary symptoms (frequency, urgency, incontinence episodes)
Rationale: To establish baseline severity and monitor treatment efficacy.
Timing: Prior to initiation of therapy
Medical history (including cardiovascular, gastrointestinal, and ophthalmologic conditions)
Rationale: To identify contraindications or conditions requiring caution (e.g., narrow-angle glaucoma, urinary retention, gastric retention, QT prolongation risk).
Timing: Prior to initiation of therapy
Renal and hepatic function tests (CrCl, LFTs)
Rationale: To determine appropriate dosing adjustments for impaired organ function.
Timing: Prior to initiation of therapy, if impairment is suspected or known
Routine Monitoring
Efficacy of symptom control (urinary frequency, urgency, incontinence)
Frequency: Periodically, e.g., every 4-8 weeks initially, then every 3-6 months
Target: Reduction in symptoms
Action Threshold: If symptoms persist or worsen, consider dose adjustment or alternative therapy.
Adverse effects (dry mouth, constipation, blurred vision, urinary retention, somnolence)
Frequency: Periodically, especially during initial weeks of therapy and after dose changes
Target: Tolerable level of side effects
Action Threshold: If severe or intolerable, consider dose reduction or discontinuation.
Post-void residual (PVR) volume
Frequency: Periodically, especially in patients at risk for urinary retention (e.g., BPH)
Target: < 100-150 mL
Action Threshold: If PVR significantly increases or symptoms of urinary retention develop, discontinue or reduce dose.
Electrocardiogram (ECG)
Frequency: Consider periodically in patients with known QT prolongation risk factors or on concomitant QT-prolonging drugs.
Target: Normal QT interval
Action Threshold: If significant QT prolongation occurs, discontinue or reduce dose.
Symptom Monitoring
- Dry mouth
- Constipation
- Blurred vision
- Urinary retention (difficulty urinating, feeling of incomplete emptying)
- Dizziness
- Somnolence
- Headache
- Abdominal pain
- Signs of allergic reaction (rash, itching, swelling)
Special Patient Groups
Pregnancy
Tolterodine is Pregnancy Category C. Studies in animals have shown adverse effects on the fetus (e.g., decreased fetal weight, increased skeletal abnormalities) at doses higher than clinical exposure. There are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Potential for teratogenicity based on animal data; human data lacking.
Second Trimester:
Limited human data; animal data suggest potential for adverse effects.
Third Trimester:
Limited human data; animal data suggest potential for adverse effects.
Lactation
It is not known whether tolterodine or its active metabolites are excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from tolterodine, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Infant Risk:
Unknown; potential for anticholinergic effects in the infant.
Pediatric Use
Safety and effectiveness in pediatric patients have not been established. Use is not recommended.
Geriatric Use
No overall differences in safety or effectiveness were observed between elderly (âĨ65 years) and younger patients. However, elderly patients may be more susceptible to anticholinergic side effects (e.g., dry mouth, constipation, cognitive impairment, urinary retention) and should be monitored closely. No specific dose adjustment is generally required based on age alone, but consider renal and hepatic function.
Clinical Information
Clinical Pearls
- Detrol LA is an extended-release formulation, designed for once-daily dosing, which can improve patient adherence compared to immediate-release formulations.
- The active metabolite, 5-hydroxymethyl tolterodine, contributes significantly to the pharmacological effect, especially in extensive CYP2D6 metabolizers.
- Patients who are poor CYP2D6 metabolizers will have higher exposure to the parent drug (tolterodine) and lower exposure to the active metabolite, but the overall clinical effect is similar.
- Counsel patients on managing common anticholinergic side effects like dry mouth (sugar-free candy/gum, sips of water) and constipation (fiber, fluids).
- Always assess for pre-existing conditions like narrow-angle glaucoma, urinary retention, or gastric retention before prescribing, as these are contraindications.
- Be cautious when co-administering with other anticholinergic drugs or drugs that prolong the QT interval.
Alternative Therapies
- Other antimuscarinic agents (e.g., oxybutynin, solifenacin, darifenacin, fesoterodine, trospium)
- Beta-3 adrenergic agonists (e.g., mirabegron, vibegron)
- OnabotulinumtoxinA (Botox) injections into the detrusor muscle
- Percutaneous tibial nerve stimulation (PTNS)
- Sacral neuromodulation (SNS)
- Behavioral therapies (e.g., bladder training, pelvic floor muscle exercises, fluid management)
Cost & Coverage
Average Cost:
$150 - $300 per 30 capsules
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (for generic), Tier 3 or higher (for brand)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist. If you have any questions or concerns about this medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide detailed information about the overdose, including the medication taken, the amount, and the time it occurred.